Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazine Ring Of The Quinazoline Ring System Patents (Class 514/266.3)
  • Patent number: 10906907
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of preparing such compounds are also disclosed, including the preparation and use of the compound tert-butyl (S)-(1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl)carbamate of formula (110) as a precursor to synthesize an exemplary compound disclosed in this application, (S)-2-(1-((9H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: May 21, 2019
    Date of Patent: February 2, 2021
    Assignee: ICOS CORPORATION
    Inventors: Edward A. Kesicki, Kerry W. Fowler, Danwen Huang, Hua Chee Ooi, Amy Oliver, Kamal Deep Puri, Fuqiang Ruan, Jennifer A. Treiberg
  • Patent number: 10590115
    Abstract: Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: March 17, 2020
    Assignee: Pfizer Inc.
    Inventors: Simon Planken, Hengmiao Cheng, Michael Raymond Collins, Jillian Elyse Spangler, Alexei Brooun, Andreas Maderna, Cynthia Palmer, Maria Angelica Linton, Asako Nagata, Ping Chen
  • Patent number: 10577369
    Abstract: The present invention relates to novel quinazolinone derivatives inhibiting PI3K; a method for preparing the derivatives; and a pharmaceutical composition for treating hematologic neoplasms or liver diseases, containing the quinazolinone derivatives, wherein the novel quinazolinone derivatives according to the present invention have a beneficial effect in the treatment of hematologic neoplasms or liver diseases. Particularly, the quinazolinone derivatives inhibit PI3K? with high selectivity compared to that of a conventional anticancer drug of PI3K? inhibitors, thereby significantly reducing immunotoxicity, or simultaneously inhibit PI3K? and PI3K?, thereby enabling the treatment of autoimmune diseases, and anticancer therapy for blood cancer and the like. These targeted drugs have reduced side effects. The present invention provides a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein X is —H, halogen, —CH3, or —NH2; and Y is C1-2 linear alkyl or C3-4 cycloalkyl.
    Type: Grant
    Filed: January 10, 2019
    Date of Patent: March 3, 2020
    Assignee: BIOWAY., INC
    Inventors: Jongwoo Kim, Chiwoo Lee, Suji Hong
  • Patent number: 10456405
    Abstract: Provided are a compound of the formula below, and a pharmaceutically acceptable salt or stereoisomer thereof that can be used for treating cardiovascular diseases and compositions containing the compounds. The compounds, a pharmaceutically acceptable salt or stereoisomer thereof and the compositions can improve lipid metabolism disorders by increasing high-density lipoprotein cholesterol in blood; in addition, the compounds, a pharmaceutically acceptable salt or stereoisomer thereof and the compositions can also release nitric oxide, and reduce the onset risk of cardiovascular diseases by means of relaxing blood vessels, lowering blood pressure, inhibiting platelet adhesion and aggregation and maintaining vascular tension, and thus play an important role in preventing and treating the occurrence and development of cardiovascular diseases.
    Type: Grant
    Filed: September 6, 2016
    Date of Patent: October 29, 2019
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD, SHANGHAI SYNERGY PHARMACEUTICAL SCIENCES CO., LTD
    Inventors: Jian Ge, Yunfei Li, Zhen Zhang, Yijin Wang, Jiamiao Wang, Tao Cheng
  • Patent number: 10369162
    Abstract: The purpose of the present invention is to identify a migratory factor that guides pluripotent stem cells (Muse cells) useful in new medical applications to damage, and to provide a pharmaceutical composition that includes the migratory factor for promoting tissue regeneration in regenerative medicine that makes use of Muse cells. In the present invention, a receptor that is specifically expressed in Muse cells rather than non-Muse cells was identified, and it was confirmed that a ligand for this receptor can function as a migratory factor. In the present invention, sphingosine-1-phosphate (S1P) was identified as a migratory factor, and thus, the present invention pertains to a pharmaceutical composition for guiding pluripotent stem cells to damage, the composition including S1P as an active ingredient.
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: August 6, 2019
    Assignees: CLIO, INC., TOHOKU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Mari Dezawa, Yoshinori Fujiyoshi, Masanori Yoshida
  • Patent number: 10336756
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of preparing such compounds are also disclosed, including the use of (S)-2-(1-aminopropyl)-5-fluoro-3-phenylquinazolin-4(3H)-one as a precursor to synthesize an exemplary compound disclosed in this application, (S)-2-(1-((9H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: July 2, 2019
    Assignee: ICOS CORPORATION
    Inventors: Edward A. Kesicki, Kerry W. Fowler, Danwen Huang, Hua Chee Ooi, Amy Oliver, Kamal Deep Puri, Fuqiang Ruan, Jennifer Treiberg
  • Patent number: 10208044
    Abstract: The present invention provides for compounds of formula I as acetyl-CoA carboxylase (ACC) inhibitors. The ACC inhibitors are useful for the prevention or treatment of metabolic syndrome, including obesity, dyslipidemia and hyperlipidemia in humans. The inhibitor compounds are also capable of inhibiting the ACC enzyme found in plants, parasites and bacteria.
    Type: Grant
    Filed: May 8, 2014
    Date of Patent: February 19, 2019
    Assignee: GILEAD APOLLO, LLC
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, George Borg, Craig E. Masse
  • Patent number: 10166234
    Abstract: The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: The pharmaceutical preparation is excellent in the solubility and the storage stability even if the amount of the compound or the salt included in each individual dosage unit is increased.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: January 1, 2019
    Assignee: EA Pharma Co., Ltd.
    Inventors: Satoshi Aburatani, Hirokazu Hagio, Hiroyuki Higuchi, Kenichi Ogawa
  • Patent number: 10123999
    Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, Cl, or X2 is H, Br, Cl, or n1 is 1-2; and n2 is 1-2.
    Type: Grant
    Filed: November 10, 2016
    Date of Patent: November 13, 2018
    Assignee: Exelixis, Inc.
    Inventor: Jo Ann Wilson
  • Patent number: 10039763
    Abstract: The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: The pharmaceutical preparation is excellent in the solubility and the storage stability even if the amount of the compound or the salt included in each individual dosage unit is increased.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: August 7, 2018
    Assignee: EA Pharma Co., Ltd.
    Inventors: Satoshi Aburatani, Hirokazu Hagio, Hiroyuki Higuchi, Kenichi Ogawa
  • Patent number: 9877970
    Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: January 30, 2018
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
  • Patent number: 9827248
    Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: November 28, 2017
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
  • Patent number: 9593083
    Abstract: The present invention provides process for preparation of Crystalline Erlotinib HCl (I) Form-SE characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2?° peaks selected from the XRPD peak set of 5.60, 10.00, 11.40, 13.00, 13.50, 15.20, 18.40, 20.65, 21.86, 23.5, 31.80, 32.13, 32.80, 34.40±0.20 2?°, DSC isotherm comprising the endothermic peaks ranging between 213 to 217° C. (Peak ?1) and 225 to 235° C. (Peak ?2) and IR absorption characteristic peaks at approximately 3278 cm?1, 1948 cm?1, 1871 cm?1, 1632 cm?1, 1164 cm?1, 1024 cm?1, 940 cm?1 and 742 cm?1 useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment cancer.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: March 14, 2017
    Assignee: SHILPA MEDICARE LIMITED
    Inventors: Vimal Kumar Shrawat, Prashant Purohit, Rafiuddin Dr., Vinod Kumar Singh, Akshay Kant Chaturvedi
  • Patent number: 9546150
    Abstract: The present invention relates to quinazolin-4-one compounds of formula (I?), their process of preparation and uses thereof. These compounds are useful as selective and reversible inhibitors of ubiquitin specific proteases, particularly USP7, for treating e.g. cancer, neurodegenerative diseases, inflammatory disorders and viral infections.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: January 17, 2017
    Assignee: HYBRIGENICS SA
    Inventors: Frédéric Colland, Marie-Edith Gourdel
  • Patent number: 9340515
    Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: May 17, 2016
    Assignee: Generics (UK) Limited
    Inventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
  • Publication number: 20150141400
    Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 21, 2015
    Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
  • Patent number: 9034887
    Abstract: A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: May 19, 2015
    Assignee: F2G Limited
    Inventors: Jason David Oliver, John Leslie Thain, Michael John Bromley, Graham Edward Morris Sibley, Michael Birch
  • Publication number: 20150133434
    Abstract: The present disclosure provides compositions and methods for reactivating latent immunodeficiency vims. The methods generally involve contacting an HIV-infected cell in which HIV is latent with an agent that binds a bromodomain (BRD) in the cell. Latently infected cells contain replication-competent integrated HIV-1 genomes that are blocked at the transcriptional level, resulting in the absence of viral protein expression. The present disclosure provides methods for reducing the reservoir of latent immunodeficiency virus in an individual.
    Type: Application
    Filed: March 13, 2013
    Publication date: May 14, 2015
    Inventors: Melanie Ott, Eric M. Verdin, Ming-Ming Zhou
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Publication number: 20150119411
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus.
    Type: Application
    Filed: June 5, 2013
    Publication date: April 30, 2015
    Inventors: Jennifer E. Golden, Jeffrey Aube, Denise S. Simpson, Daniel P. Flaherty, Daljit S. Matharu, William E. Severson, Lynn Rasmussen
  • Publication number: 20150110723
    Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.
    Type: Application
    Filed: May 28, 2013
    Publication date: April 23, 2015
    Applicant: EMORY UNIVERSITY
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Patent number: 9006257
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: April 14, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram Gharat, Abhisek Banerjee, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Patent number: 8993583
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 31, 2015
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Publication number: 20150087636
    Abstract: The use of BETi as a potential treatment for FSHD is provided. Specifically, the use of BETi, and particularly selective BETi for BRD4, are shown to inhibit DUX4 expression which is expected to result in a decrease in the severity of symptoms of FSHD. Further, the treatments are shown to work when pulsed as opposed to continuous. This allows for a BETi to be supplied to a human in a pulse, and then allows the human to not need any additional treatment for a window at least as long as the one of the treatment pulse.
    Type: Application
    Filed: September 19, 2014
    Publication date: March 26, 2015
    Inventor: Francis M. Sverdrup
  • Patent number: 8980901
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 17, 2015
    Assignee: Icos Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Patent number: 8969325
    Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: March 3, 2015
    Assignee: AbbVie Inc.
    Inventors: Michael J. Dart, Philip R. Kym, Eric A. Voight, Anurupa Shrestha, Jerome F. Daanen, Tammie K. Jinkerson, Ryan G. Keddy, Sridhar Peddi, Arthur Gomtsyan, Michael E. Kort, Gregory A. Gfesser, Kevin R. Woller, Derek W. Nelson
  • Patent number: 8962639
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, X, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: February 24, 2015
    Assignee: AbbVie Inc.
    Inventors: Marc J. Scanio, William H. Bunnelle, William A. Carroll, Sridhar Peddi, Arturo Perez-Medrano, Lei Shi
  • Patent number: 8957087
    Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: February 17, 2015
    Assignees: Jiangsu Provincial Institute of Materia Medica Co., Ltd., Nanjing Luyesike Pharmaceutical Co., Ltd.
    Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
  • Patent number: 8952021
    Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: February 10, 2015
    Assignee: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Patent number: 8952022
    Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: February 10, 2015
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
  • Publication number: 20150025072
    Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).
    Type: Application
    Filed: October 7, 2014
    Publication date: January 22, 2015
    Applicant: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Penelope Jane HUGGINS, Jack Gordon PARSONS
  • Patent number: 8937078
    Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: January 20, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, Jr., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Publication number: 20150018371
    Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
  • Publication number: 20150017262
    Abstract: The present invention relates to compositions and methods for reducing cell proliferation and/or promoting cell death by inhibiting Drp1. It is based, at least in part, on the discoveries that (i) Drp1 disruption-induced mitochondrial hyperfusion is functionally linked to the cell cycle regulation apparatus, so that Drp1 inhibition results in a disruption of the cell cycle and DNA aberrancies; (ii) inhibition of both Drp1 and ATR are synthetic lethal causing increased DNA damage and apoptotic cell death; and (iii) even in resistant cell lines, Drp1 inhibitor (e.g., mdivi-1) together with a second antiproliferative agent (e.g., cisplatin or carboplatin) act synergistically to promote apoptosis. Accordingly, the present invention provides for novel anticancer strategies.
    Type: Application
    Filed: May 8, 2014
    Publication date: January 15, 2015
    Applicant: University of Pittsburgh - of the Commonwealth System of Higher Education
    Inventors: Wei Qian, Bennett Van Houten
  • Patent number: 8927559
    Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, Jr., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Purakkattle Johny Biju, Li Dong, Xianhai Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi, Ashwin U. Rao
  • Publication number: 20150005327
    Abstract: The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventor: Thomas Helleday
  • Publication number: 20140357652
    Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, JR., Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
  • Patent number: 8901135
    Abstract: Substituted bicyclic heteroaryls having the following formula where the variables are as defined herein, and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-pro
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: December 2, 2014
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140350033
    Abstract: ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrimidinone of formula I wherein R1 is —(CH2)n-CO—OH; —(CH2)n-CO—OR; —(CH2)n-CO—NHR; —(CH2)n-CO—N(R, R?); —(CH2)n-OH; —(CH2)n-OR; —(CH2)n-OAr; —(CH2)n-C(R,R?)—(CH2)n-OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.
    Type: Application
    Filed: June 5, 2014
    Publication date: November 27, 2014
    Applicants: MITOLOGICS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE VERSAILLES-SAINT QUENTIN-EN-YVELINES (UVSQ)
    Inventors: Annie BORGNE-SANCHEZ, Etienne JACOTOT, Catherine BRENNER
  • Publication number: 20140315932
    Abstract: The present specification relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Applicant: NOVARTIS AG
    Inventors: Timothy John RITCHIE, Andrew James CULSHAW, Christopher Thomas BRAIN, Edward Karol DZIADULEWICZ, Terance William HART
  • Publication number: 20140275711
    Abstract: Disclosed are novel 1-(arylmethyl)-5,6,7,8-tetrahydroquinazoline-2,4-diones and analogs thereof, represented by the Formula I, wherein Ar, A, B, R3-R6 are defined herein. Compounds having Formula I are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity, such as cancer.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 18, 2014
    Inventors: Suixiong Cai, Ye Edward Tian, Lizhen Wu, Lijun Liu, Xiaozhu Wang, Yangzhen Jiang, Guoxiang Wang, Xiuyan Zhang, Qingbing Xu, Zheng Meng
  • Publication number: 20140256753
    Abstract: Provided is a process for treating or preventing a viral infection in a subject, wherein the viral infection is from a flavivirus selected from the group consisting of Hepatitis C Virus (genotypes 1-7) and Japanese Encephalitis Virus.
    Type: Application
    Filed: August 10, 2012
    Publication date: September 11, 2014
    Applicants: Sanford-Burnham Medical Research Institute, Southern Research Institute
    Inventors: Marintha L. Heil, Nicholas D.P. Cosford, Robert Ardecky, Jiwen Zou
  • Publication number: 20140249151
    Abstract: [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11?-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11?-HSD1.
    Type: Application
    Filed: October 17, 2012
    Publication date: September 4, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shimpei Kawakami, Minoru Sakurai, Noriyuki Kawano, Takayuki Suzuki, Nobuyuki Shiraishi, Wataru Hamaguchi, Ryuichi Sekioka, Hiroyuki Moritomo, Ayako Motitomo
  • Patent number: 8815878
    Abstract: Substituted spiro hemiaminals and methods for their use in the treatment of viral diseases, including hepatitis C viral infections, are described herein.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: August 26, 2014
    Assignee: NovaDrug, LLC
    Inventor: Eliezer Huberman
  • Patent number: 8802666
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 12, 2014
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140221201
    Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one active compound II selected from a group M comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, allosteric nicotinic acetylcholine receptor activators, chloride channel activators, juvenile hormone mimics, homopteran feeding blockers, mit grow inhibitors, inhibitors of mitochondrial bATP synthase, uncouplers of the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, ecdyson receptor agonists, octamin receptor agonists, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis, ryanodine receptor modulators and other compounds as defined in the description, in syne
    Type: Application
    Filed: August 30, 2012
    Publication date: August 7, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Steffen Groß, Jürgen Langewald, Arun Narine
  • Publication number: 20140221298
    Abstract: The present invention provides an agricultural and horticultural fungicidal composition including a compound A which is at least one selected from a nitrogen-containing heterocyclic compound having a specific structure including a compound represented by the formula (1), and a salt thereof, and a compound B which is at least one selected from the group of specific pesticidally active compounds: in the formula (1), X each independently represents a halogeno group or a C1 to 6 alkyl group; n represents the number of X(s) and is an integer of 0 to 6; and X? represents a halogeno group; and R1, R2 and R3 each independently represent a C1 to 6 alkyl group or a hydroxyl group.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 7, 2014
    Inventor: Raito Kuwahara
  • Publication number: 20140213445
    Abstract: The present invention relates to agricultural methods and the use of 3-arylquinazolin-4-one derivatives of formula (I) wherein R1, R2, R3, R4, k and n are defined in the description in soil application methods. The compounds of the formula (I) are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.
    Type: Application
    Filed: August 31, 2012
    Publication date: July 31, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Steffen Gross, Arun Narine, Koshi Gunjima